Z218484536
Based on 1 Customer Validation
Z218484536 is a selective and brain-penetrant phosphoserine phosphatase (PSPH) inhibitor. Z218484536 binds to PSPH with a Kd value of approximately 0.23 μM. Z218484536 reduces L-serine and D-serine levels in astrocytes. Z218484536 is able to suppress spontaneous epileptic seizures without causing serious side effects. Z218484536 also shows good anti-epileptic effects in the temporal lobe epilepsy (TLE) model.
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- Pureza: 97.65%
- No. CAS: 1223877-07-3
- Fòrmula: C11H10FN5O
- Peso molecular:247.23
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Z218484536 (40-2,000 nM, 24 h) inhibits the release of l-serine, with an IC50 of 0.4 μM, and reduces cellular L-serine levels with an IC50 of 0.38 μM in cultured astrocytes[1].
Z218484536 (0.078-40 μM, 48 h) has no toxic effect on the proliferation of HepG2 cells[1].MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUClast | T1/2 | Tmax | Cmax | AUCINF_obs | MRTlast | MRTINF_obs |
|---|---|---|---|---|---|---|---|---|---|
| Mice | 4 mg/kg | i.p. | 1088.34 ng·h/mL | 2.71 h | 0.17 h | 1420.54 ng/mL | 1100.16 ng·h/mL | 1.00 h | 1.17 h |
Z218484536 (0.5-20 mg/kg, i.p., once a day, 3 day) delays the onset of acute epilepsy, reduces the severity of seizures, and is anticonvulsant in a Pentylenetetrazole (PTZ) -induced acute epilepsy model[1].
Z218484536 (2 mg/kg, 4 mg/kg, i.p., once a day 3 day) reduces hippocampal L-serine and D-serine levels in a Kainic acid (HY-N2309) (KA)-induced chronic TLE mouse model[1].
Z218484536 (2 mg/kg, 4 mg/kg, i.p., once a day, 7 weeks) suppresses spontaneous seizures in TLE mice[1].
Z218484536 (4 mg/kg, i.p., once a day, 7 day) not affect the mice's emotional state or motor ability[1].
Z218484536 (1 mg/kg, 2 mg/kg, i.p.,2 weeks, once a day, 3.5 months) reduces epileptic activity in a cynomolgus monkey TLE model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KA mouse model of chronic TLE[1]
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Dosage:2 mg/kg, 4 mg/kg
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Administration:i.p., 7 weeks, once a day
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Result:Reduced SES frequency to 0.44 per day .
Not caused weight loss.
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Animal Model:PTZ-induced acute model of seizures[1]
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Dosage:0.5 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg, 20 mg/kg
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Administration:i.p., 3 days, once a day
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Result:Delayed the onset of acute epilepsy .
The maximum anticonvulsant effect was observed at a concentration of 4 mg/kg
Chemical Information
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No. CAS 1223877-07-3
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Appearance Solid
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Peso molecular 247.23
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Fòrmula C11H10FN5O
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Color White to off-white
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SMILES
O=C(N/N=C/C1=CNN=C1C2=CC=C(F)C=C2)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 100 mg/mL (404.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.0448 mL | 20.2241 mL | 40.4482 mL | 101.1204 mL |
| 5 mM | 0.8090 mL | 4.0448 mL | 8.0896 mL | 20.2241 mL | |
| 10 mM | 0.4045 mL | 2.0224 mL | 4.0448 mL | 10.1120 mL | |
| 15 mM | 0.2697 mL | 1.3483 mL | 2.6965 mL | 6.7414 mL | |
| 20 mM | 0.2022 mL | 1.0112 mL | 2.0224 mL | 5.0560 mL | |
| 25 mM | 0.1618 mL | 0.8090 mL | 1.6179 mL | 4.0448 mL | |
| 30 mM | 0.1348 mL | 0.6741 mL | 1.3483 mL | 3.3707 mL | |
| 40 mM | 0.1011 mL | 0.5056 mL | 1.0112 mL | 2.5280 mL | |
| 50 mM | 0.0809 mL | 0.4045 mL | 0.8090 mL | 2.0224 mL | |
| 60 mM | 0.0674 mL | 0.3371 mL | 0.6741 mL | 1.6853 mL | |
| 80 mM | 0.0506 mL | 0.2528 mL | 0.5056 mL | 1.2640 mL | |
| 100 mM | 0.0404 mL | 0.2022 mL | 0.4045 mL | 1.0112 mL |
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